- NURR1 RECEPTOR MODULATORS
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Described herein, inter alia, are Nurr1 receptor modulators and uses thereof. In an aspect is provided a method for treating a disease associated with dysregulation and/or degeneration of dopaminergic neurons in the central nervous system of a subject in need thereof, the method including administering to the subject in need thereof a therapeutically effective amount of a compound described herein.
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Paragraph 0646; 1262-1264
(2020/09/08)
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- N -Arylation of (hetero)arylamines using aryl sulfamates and carbamates via C-O bond activation enabled by a reusable and durable nickel(0) catalyst
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An effective and general aryl amination protocol has been developed using a magnetically recoverable Ni(0) based nanocatalyst. This new stable catalyst was prepared on Fe3O4@SiO2 modified by EDTA and investigated by FT-IR, EDX, TEM, XRD, DLS, FE-SEM, XPS, NMR, TGA, VSM, ICP and elemental analysis techniques. The reaction proceeded via carbon-oxygen bond cleavage of (hetero)aryl carbamates and sulfamates under simple and mild conditions without the use of any external ligands. This method demonstrated functional group tolerance in the N-arylation of various nitrogen-containing compounds as well as aliphatic amines, anilines, pyrroles, pyrazoles, imidazoles, indoles, and indazoles with good to excellent yields. Furthermore, the catalyst could be easily recovered by using an external magnetic field and directly reused at least six times without notable reduction in its activity. This journal is
- Dindarloo Inaloo, Iman,Majnooni, Sahar,Eslahi, Hassan,Esmaeilpour, Mohsen
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p. 13266 - 13278
(2020/10/07)
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- Development of a Scalable Process for the Insecticidal Candidate Tyclopyrazoflor. Part 1. Evaluation of [3 + 2] Cyclization Strategies to 3-(3-Chloro-1 H-pyrazol-1-yl)pyridine
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The evaluation of [3 + 2] cyclization strategies to prepare a key intermediate, 3-(3-chloro-1H-pyrazol-1-yl)pyridine, for the insecticidal candidate tyclopyrazoflor (1) is described. Among the validated strategies, the route involving [3 + 2] cyclization of 3-hydrazinopyridine·2HCl with methyl acrylate was selected for further optimization. This route provided ready access to 3-(3-chloro-1H-pyrazol-1-yl)pyridine in three steps via cyclization, chlorination, and oxidation. Further functionalization of 3-(3-chloro-1H-pyrazol-1-yl)pyridine via nitration, reduction, and amide formation with 3-((3,3,3-trifluoropropyl)thio)propanoic acid followed by ethylation rendered 1 in a total of seven steps.
- Yang, Qiang,Li, Xiaoyong,Lorsbach, Beth A.,Roth, Gary,Podhorez, David E.,Ross, Ronald,Niyaz, Noormohamed,Buysse, Ann,Knueppel, Daniel,Nissen, Jeffrey
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p. 2122 - 2132
(2019/11/02)
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- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
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This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
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Paragraph 0191; 0192
(2016/05/02)
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- N-(1-Oxy-2-picolyl)oxalamic acids as a new type of O,O-ligands for the Cu-catalyzed N-arylation of azoles with aryl halides in water or organic solvent
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N-(1-Oxy-pyridin-2-ylmethyl)oxalamic acids (L3-L5) were identified as novel efficient ligands for copper-catalyzed C-N cross-coupling of azoles and aryl halides in water. The N-arylation of imidazoles, indoles and pyrazoles proceeded with moderate to excellent yields and complete selectivity over aromatic amines and phenols. Moreover, L5, which is also efficient in organic solvent with low catalyst loading, can be used to promote the N-arylation reactions with water-sensitive materials. The catalytic mechanism was proposed based on the results of several verification experiments which indicated that the ligands as new-type chelators may coordinate to Cu(i) with two oxygen atoms of N-oxide and amide in the coupling process. This journal is
- Wang, Yongbin,Zhang, Yu,Yang, Beibei,Zhang, Ao,Yao, Qizheng
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p. 4101 - 4114
(2015/03/30)
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- Ligand-free Cu2O-catalyzed cross coupling of nitrogen heterocycles with iodopyridines
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A practical and efficient strategy has been developed for the cross coupling of nitrogen heterocycles with halopyridines using ligand-free Cu 2O as catalyst and Cs2CO3 as the base. The protocol is applicable to a series of highly functionalised heterocycles, such as 7-azaindole, indazole, indole, imidazole, pyrrole and pyrazole, affording the N-heteroaryl derivatives in high yields (up to 96%).
- Teo, Yong-Chua,Yong, Fui-Fong,Sim, Shirlyn
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p. 7279 - 7284
(2013/08/23)
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- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
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This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
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Paragraph 0163; 0164
(2013/05/09)
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- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
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This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
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Paragraph 0191-0192
(2013/11/06)
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- PESTICIDAL COMPOSTIONS AND PROCESSES RELATED THERETO
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This document discloses pesticidal molecules having the following formula (“Formula One”): and processes related thereto.
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Paragraph 0164; 0165
(2013/03/26)
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- A convenient synthesis of (1 H-azol-1-yl)piperidines
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A convenient preparation of 3- and 4-(1H-azol-1-yl)piperidines by arylation of azoles (i.e., pyrazoles, imidazoles, and triazoles) with 3- and 4-bromopyridines and subsequent reduction of the pyridine ring was developed. The method was extended to benzo analogues of the title compounds. Georg Thieme Verlag Stuttgart · New York.
- Shevchuk, Nadiia V.,Liubchak, Kostiantyn,Nazarenko, Kostiantyn G.,Yurchenko, Aleksandr A.,Volochnyuk, Dmitriy M.,Grygorenko, Oleksandr O.,Tolmachev, Andrey A.
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experimental part
p. 2041 - 2048
(2012/08/07)
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- Pesticidal Compositions and Processes Related Thereto
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This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
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Page/Page column 15
(2012/05/07)
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- Microwave-assisted solvent- and ligand-free copper-catalysed cross-coupling between halopyridines and nitrogen nucleophiles
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N-Heteroarylated products are obtained in good yields by microwave-assisted solvent- and ligand-free copper-catalysed amination of halopyridines with nitrogen nucleophiles.
- Liu, Zhen-Jiang,Vors, Jean-Pierre,Gesing, Ernst R. F.,Bolm, Carsten
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supporting information; experimental part
p. 42 - 45
(2011/03/19)
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- N-aryl pyrazoles: DFT calculations of CH acidity and deprotonative metallation using a combination of lithium and zinc amides
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A series of N-aryl and N-heteroaryl pyrazoles have been deproto-metallated using a 2,2,6,6-tetramethylpiperidino-based mixed lithium-zinc combination. Mono-, di-, and tri-iodides have been obtained after subsequent trapping with iodine, depending on the s
- Chevallier, Floris,Halauko, Yury S.,Pecceu, Christelle,Nassar, Ibrahim F.,Dam, To Uyen,Roisnel, Thierry,Matulis, Vadim E.,Ivashkevich, Oleg A.,Mongin, Florence
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scheme or table
p. 4671 - 4684
(2011/07/07)
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- Transition-metal-free O-,S -, and N-arylation of alcohols, thiols, amides, amines, and related heterocycles
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A new protocol for the Ullmann-type arylation process of different aromatic heterocycles without any transition-metal catalyst, implying the use of a combination of an excess of potassium hydroxide and dimethyl sulfoxide, is described. The reaction can be performed between a broad range of starting nucleophiles including phenol, alcohols, amines, nitrogen-containing five-membered systems such as pyrazoles, imidazoles, and indoles, and amides with haloarenes, iodide and bromide derivatives giving the best results, the possible pathway involving the in situ generation of the corresponding benzyne intermediate. When the reaction was performed with 2-iodoaniline and either carboxamides or isothiocyanato derivatives, the corresponding benzoazole derivatives were obtained.
- Cano, Rafael,Ramon, Diego J.,Yus, Miguel
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experimental part
p. 654 - 660
(2011/03/20)
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- Ligand-free copper-catalyzed amination of heteroaryl halides with alkyl- and arylamines
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N-Heteroarylations of alkyl- and arylamines with various heteroaryl halides have been achieved by ligand-free copper-catalyzed cross-couplings affording aminopyridines and aminopyrimidines in moderate to high yields (up to 99% yield). Copyright
- Liu, Zhen-Jiang,Vors, Jean-Pierre,Gesing, Ernst R. F.,Bolm, Carsten
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supporting information; experimental part
p. 3158 - 3162
(2011/02/26)
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- Iron complex-catalyzed N-arylation of pyrazoles under aqueous medium
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Commercially available FeCl3·6H2O with conformationally rigid diamine ligand is a highly effective catalyst for N-arylation of pyrazoles using aryl and heteroaryl iodides. It is notable to show that this complex is tolerable under aqueous medium and particularly the whole reaction utilizes water as the sole solvent without any additional organic co-solvents and surfactants. Attempted study using other nitrogen nucleophiles is described. This newly developed system provides an alternative protocol to Cu- and Pd-catalyzed N-arylation reactions.
- Lee, Hang Wai,Chan, Albert S.C.,Kwong, Fuk Yee
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experimental part
p. 5868 - 5871
(2010/01/11)
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- Mild conditions for copper-catalysed N-arylation of pyrazoles
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Copper-catalysed N-arylation of pyrazoles with aryl or heteroaryl bromides or iodides, which can include functional substituents, was performed under the mildest conditions yet described, with excellent yields and selectivity, by the use as catalyst of a combination of cuprous oxide with a set of inexpensive, chelating oxime-type ligands not previously known to promote such reactions. Other original bi-, tri- or tetradentate ligands providing nitrogen and/or oxygen as chelating atoms were also successfully tested in this type of arylation. ( Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004).
- Cristau, Henri-Jean,Cellier, Pascal P.,Spindler, Jean-Francis,Taillefer, Marc
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p. 695 - 709
(2007/10/03)
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